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公开(公告)号:US20060135770A1
公开(公告)日:2006-06-22
申请号:US11315528
申请日:2005-12-22
申请人: Muhammad Javaid , Graeme Smith , Niall Martin , Sylvie Gomez , Vincent Loh , Xiao-Ling Cockcroft , Keith Menear
发明人: Muhammad Javaid , Graeme Smith , Niall Martin , Sylvie Gomez , Vincent Loh , Xiao-Ling Cockcroft , Keith Menear
IPC分类号: C07D403/14
CPC分类号: C07C235/60 , C07C2601/08 , C07C2601/14 , C07D207/08 , C07D215/36 , C07D231/14 , C07D231/18 , C07D231/20 , C07D241/44 , C07D261/10 , C07D261/18 , C07D263/32 , C07D271/12 , C07D277/18 , C07D295/14 , C07D295/18 , C07D295/26 , C07D307/14 , C07D307/52 , C07D317/68 , C07D333/34 , C07D333/62 , C07D401/06 , C07D403/06 , C07D413/06 , C07D495/04
摘要: A compound of the formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R2, R3, R4 and R5 are independently selected from the group consisting of H, C1-7 alkoxy, amino, halo or hydroxy; n is 1 or 2; RN1 and RN2 are independently selected from H and R, where R is optionally substituted C1-10 alkyl, C3-20 heterocyclyl and C5-20 aryl; or RN1 and RN2, together with the nitrogen atom to which they are attached form an optionally substituted 5-7 membered, nitrogen containing, heterocylic ring; Het is selected from: where Y1 and Y3 are independently selected from CH and N, Y2 is selected from CX and N and X is H, Cl or F; and where Q is O or S.
摘要翻译: 式(I)的化合物及其异构体,盐,溶剂合物,化学保护形式及其前药,其中:R 2,R 3,R 3, 4和R 5独立地选自H,C 1-7烷氧基,氨基,卤素或羟基; n为1或2; R N1和R N2独立地选自H和R,其中R是任选取代的C 1-10烷基,C 3 -20个杂环基和C 5-20-20芳基; 或R N1和R N2,以及它们所连接的氮原子一起形成任选取代的5-7元含氮杂环; Het选自:其中Y 1和Y 3独立地选自CH和N,Y 2选自CX和N和X 是H,Cl或F; 而Q是O或S.
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公开(公告)号:US20070093489A1
公开(公告)日:2007-04-26
申请号:US11550004
申请日:2006-10-17
申请人: Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
发明人: Muhammad Javaid , Keith Menear , Sylvie Gomez , Marc Hummersone , Niall Martin , Graeme Smith , Xiao-Ling Cockcroft
IPC分类号: A61K31/53
CPC分类号: C07D403/10 , C07D403/14 , C07D411/14 , C07D413/14 , C07D487/04
摘要: A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; D is selected from: (i) where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N; and (ii) and where Q is O or S; RD is: wherein RN1 is selected from H and optionally substituted C1-10 alkyl; X is selected from a single bond, NRN2, CRC3RC4 and C═O; RN2 is selected from H and optionally substituted C1-10 alkyl; RC3 and RC4 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; Y is selected from NRN3 and CRC1RC2; RC1 and RC2 are independently selected from H, R, C(═O)OR, where R is optionally substituted C1-10 alkyl, optionally substituted C5-20 aryl or optionally substituted C3-20 heterocyclyl; RC1 and RC2 together with the carbon atom to which they are attached may form an optionally substituted spiro-fused C5-7 carbocylic or heterocyclic ring; and when X is a single bond RN1 and RC2 may together with the N and C atoms to which they are bound, form an optionally substituted C5-7 heterocylic ring; and when X is CRC3RC4, RC2 and RC4 may together form an additional bond, such that there is a double bond between the atoms substituted by RC1 and RC3.
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公开(公告)号:US20060063767A1
公开(公告)日:2006-03-23
申请号:US11213504
申请日:2005-08-26
申请人: Muhammad Javaid , Graeme Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Cockcroft , Stefano Forte , Keith Menear , Ian Timothy William Matthews
发明人: Muhammad Javaid , Graeme Smith , Niall Morrison Barr Martin , Sylvie Gomez , Vincent Junior Ming-lai Loh , Xiao-Ling Cockcroft , Stefano Forte , Keith Menear , Ian Timothy William Matthews
IPC分类号: A61K31/502 , C07D403/02
CPC分类号: C07D401/06 , C07D401/14 , C07D405/06 , C07D409/06 , C07D409/14 , C07D417/06
摘要: A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; and where Q is O or S.
摘要翻译: 式(I)的化合物:
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公开(公告)号:US20060149059A1
公开(公告)日:2006-07-06
申请号:US11318155
申请日:2005-12-23
申请人: Niall Martin , Graeme Smith , Stephen Jackson , Vincent Loh , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Frank Kerrigan , Alan Ashworth
发明人: Niall Martin , Graeme Smith , Stephen Jackson , Vincent Loh , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Frank Kerrigan , Alan Ashworth
IPC分类号: C07D403/02 , A61K31/502
CPC分类号: A61K31/00 , C07D237/32 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D491/04 , C07D495/04
摘要: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.
摘要翻译: 式(I)的化合物:其中A和B一起表示任选取代的稠合芳环; X可以是NR X或X X R O Y; 如果X = NR X,则n为1或2,并且如果X = CR X R Y Y,则n为1; R X选自H,任选取代的C 1-20烷基,C 5-20-20芳基,C 1〜 酰胺基,磺酰基,磺酰基,酰基和磺酰基; R Y选自H,羟基,氨基; 或R X和R Y可以一起形成螺C 3-7环烷基或杂环基; R C1和R C2都是氢,或者当X是CR X R Y,R O, C 1,R 2,R 2,X和R Y以及它们所连接的碳原子可以形成 任选取代的稠合芳环; R 1和R 2选自H和卤素。
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公开(公告)号:US20060199804A1
公开(公告)日:2006-09-07
申请号:US11361599
申请日:2006-02-24
IPC分类号: A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/53 , A61K31/506 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号: C07D251/54 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/04 , C07D405/14 , C07D417/04 , C07D471/04
摘要: Compounds of formula I: A-B-C (I)and isomers, salts, solvates, chemically protected forms, and prodrugs thereof wherein: B is selected from the group consisting of: where RN is H or Me; or B is a divalent C5 heterocyclic residue containing one or two ring heteroatoms; A is: RA3 and RA5 are independently selected from halo, ORO and RAC, where RO is H or Me, and RAC is H or C1-4 alkyl; XA is selected from N and CRA4, where RA4 is selected from H, ORO, CH2OH, CO2H, NHSO2Me and NHCOMe; RA2 and RA6 are independently selected from H, halo and ORO; or RA3 and RA4 together with the carbon atoms to which they are attached, or RA2 and RA3 together with the carbon atoms to which they are attached, may form a C5-6 heterocylic or heteroaromatic ring, containing at least one nitrogen ring atom; where if X is not N, 1, 2, or 3 of RA2 to RA6 are not H; C is: where X is selected from N and CH, Y is selected from N and CH, and Z is selected from N and CRC6; RC3 is selected from H, halo and an optionally substituted N-containing C5-7 heterocyclic group; RC5 is a group selected from: which group may be selected by one or two C1-4 alkyl groups or a carboxy group; RC6 is H; or, when X and Y are N, RC5 and RC6 (when Z is CRC6) together with the carbon atoms to which they are attached may form a fused C6 aromatic ring selected from the group consisting of:
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公开(公告)号:US20060199803A1
公开(公告)日:2006-09-07
申请号:US11361213
申请日:2006-02-24
申请人: Marc Hummersone , Sylvie Gomez , Keith Menear , Xiao-Ling Cockcroft , Peter Edwards , Ming-lai Loh , Graeme Smith
发明人: Marc Hummersone , Sylvie Gomez , Keith Menear , Xiao-Ling Cockcroft , Peter Edwards , Ming-lai Loh , Graeme Smith
IPC分类号: A61K31/551 , A61K31/541 , A61K31/519 , A61K31/5377 , C07D487/02
CPC分类号: C07D471/04
摘要: Compounds of formula l: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof one of X1, X2 and X3 is N, and the others are CH; RN1 and RN2 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms; RN3 and RN4 together with the nitrogen atom to which they are attached form a nitrogen-containing heterocyclic ring having from 4 to 8 ring atoms and their use in treating diseases ameliorated by the inhibition of mTOR.
摘要翻译: 式1化合物及其异构体,盐,溶剂合物,化学保护形式及其前药之一,X 1,X 2和X 3, 是N,其他是CH; R N1和R N2与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环; R 3 N 3和R 4 N 4与它们所连接的氮原子一起形成具有4至8个环原子的含氮杂环,并且其用于治疗改善的疾病 通过抑制mTOR。
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公开(公告)号:US20060264623A1
公开(公告)日:2006-11-23
申请号:US11403763
申请日:2006-04-13
申请人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Marine Desage-El Murr
发明人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , Hilary Calvert , Nicola Curtin , Marine Desage-El Murr
IPC分类号: C07D413/00
CPC分类号: C07D413/00 , C07D401/14 , C07D405/04 , C07D407/04 , C07D407/14 , C07D409/04 , C07D471/04
摘要: Compounds of formula l: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; are disclosed for use in inhibiting DNA-PK.
摘要翻译: 式I化合物:其中A,B和D分别选自:(i)CH,NH,C; (ii)CH,N,N;和(iii)CH,O,C; 被公开用于抑制DNA-PK。
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公开(公告)号:US20070049588A1
公开(公告)日:2007-03-01
申请号:US11468315
申请日:2006-08-30
申请人: Graeme Smith , Niall Martin , Andrew Slade , Keith Menear , Marc Hummersone , Xiao-Ling Cockcroft , Ian Matthews , Laurent Rigoreau , Roger Griffin , David Newell , Nicola Curtin
发明人: Graeme Smith , Niall Martin , Andrew Slade , Keith Menear , Marc Hummersone , Xiao-Ling Cockcroft , Ian Matthews , Laurent Rigoreau , Roger Griffin , David Newell , Nicola Curtin
IPC分类号: A61K31/5377 , C07D413/14
CPC分类号: C07D409/04
摘要: A compound of formula (I): and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, and their use in treating diseases ameliorated by the inhibition of ATM.
摘要翻译: 式(I)的化合物及其异构体,盐,溶剂化物,化学保护形式及其前药,以及它们在治疗通过抑制ATM而改善的疾病中的用途。
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公开(公告)号:US20060264427A1
公开(公告)日:2006-11-23
申请号:US11403606
申请日:2006-04-13
申请人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , HiIary Calvert , Nicola Curtin , Kappusamy Saravanan , Marine Desage-El Murr
发明人: Graeme Smith , Niall Martin , Keith Menear , Marc Hummersone , Xiao-ling Cockcroft , Mark Frigerio , Roger Griffin , Bernard Golding , Ian Hardcastle , David Newell , HiIary Calvert , Nicola Curtin , Kappusamy Saravanan , Marine Desage-El Murr
IPC分类号: A61K31/541 , A61K31/5377 , C07D487/02
CPC分类号: C07D413/00 , C07D401/14 , C07D405/04 , C07D407/04 , C07D407/14 , C07D409/04 , C07D471/04
摘要: Compounds of formula I: wherein A, B and D are respectively selected from the group consisting of: (i) CH, NH, C; (ii) CH, N, N;and (iii) CH, O, C; the dotted lines represent two double bonds in the appropriate locations; and where Z is selected from S, O, C(═O), CH2 and NH are disclosed for use in inhibiting DNA-PK.
摘要翻译: 式I化合物:其中A,B和D分别选自:(i)CH,NH,C; (ii)CH,N,N;和(iii)CH,O,C; 虚线表示适当位置的两个双键; 并且其中Z选自S,O,C(-O),CH 2和NH,用于抑制DNA-PK。
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公开(公告)号:US20050054657A1
公开(公告)日:2005-03-10
申请号:US10918180
申请日:2004-08-13
申请人: Graeme Smith , Niall Martin , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Laurent Rigoreau , Marc Hummersone , Roger Griffin
发明人: Graeme Smith , Niall Martin , Xiao-Ling Cockcroft , Ian Matthews , Keith Menear , Laurent Rigoreau , Marc Hummersone , Roger Griffin
IPC分类号: A61P31/12 , A61P35/00 , C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/04 , A61K31/496 , C07D49/14
CPC分类号: C07D409/04 , C07D409/14 , C07D413/04 , C07D417/04 , C07D417/14 , C07D491/04 , C07D495/04
摘要: A compound of formula I: and isomers, salts, solvates, chemically protected forms, and prodrugs thereof, wherein: R1 and R2 together form, along with the nitrogen atom to which they are attached, an optionally substituted heterocyclic ring having from 4 to 8 ring atoms; and RN1 is selected from hydrogen, an optionally substituted C1-7 alkyl group, an optionally substituted C3-20 heterocyclyl group, an optionally substituted C5-20 aryl group, an acyl group, an ester group and an amido group, and its use as a pharmaceutical.
摘要翻译: 式I化合物及其异构体,盐,溶剂合物,化学保护形式及其前药,其中:R 1和R 2一起与它们所连接的氮原子一起形成任选取代的杂环 具有4至8个环原子的环; 并且R N1选自氢,任选取代的C 1-7烷基,任选取代的C 3-20杂环基,任选取代的C 5-20芳基,酰基,酯基和酰胺基,以及 其用作药物。
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